In vivo metabolism-based discovery of a potent cholesterol absorption inhibitor, SCH58235, in the rat and rhesus monkey through the identification of the active …
M Van Heek, CF France, DS Compton… - The Journal of …, 1997 - Elsevier
ABSTRACT SCH48461 is a selective and highly potent inhibitor of cholesterol absorption. In
rats, SCH48461 is rapidly and completely metabolized in the first pass through the body. To
compare the activity of the metabolites of SCH48461 with SCH48461 itself, an intestinally
cannulated, bile duct-cannulated rat model for cholesterol absorption was developed.
SCH48461 inhibited the absorption of cholesterol by 70%, whereas bile containing the
metabolites of SCH48461 (henceforth,“metabolite bile”) inhibited the absorption by greater …
rats, SCH48461 is rapidly and completely metabolized in the first pass through the body. To
compare the activity of the metabolites of SCH48461 with SCH48461 itself, an intestinally
cannulated, bile duct-cannulated rat model for cholesterol absorption was developed.
SCH48461 inhibited the absorption of cholesterol by 70%, whereas bile containing the
metabolites of SCH48461 (henceforth,“metabolite bile”) inhibited the absorption by greater …